Buparlisib (BKM120) is an oral
pan-PI3K inhibitor targeting all four isoforms
of class I PI3K (α, β, γ, δ)
1
In preclinical studies, buparlisib
was active in human tumor cell
lines with and without PI3K
pathway alterations
1
•
Buparlisib showed preferential inhibition of tumor cells
bearing oncogenic mutations in
PIK3CA
1
Buparlisib (BKM120) is an Oral Pan-PI3K Inhibitor
Regulatory
subunit
Catalytic subunit
(4 isoforms: α,β,γ,δ)
p110
p85
PI3K
α
β
γ
δ
Buparlisib
Pan-PI3K inhibitor
52
166 IC50 (nM)
1
262
116 IC50 (nM)
1
1. Maira SM, et al. Mol Cancer Ther 2012;11:317–328.
